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- Title
Synthesis and ex vivo autoradiographic evaluation of ethyl-β-D-galactopyranosyl-(1,4')-2'-deoxy-2'-[18F]fluoro-β-D-glucopyranoside--a novel radioligand for lactose-binding protein: implications for early detection of pancreatic carcinomas with PET.
- Authors
Yunming Ying; Ghosh, Pradip; Liwei Guo; Pal, Ashutosh; Mukhapadhyay, Uday; Zhenghong Peng; Hsin Hsien Yeh; Bertolini, Susanna; Flores, Leo Garcia; Young, Daniel; Volgin, Andrei; Soghomonyan, Suren; Bornmann, William; Logsdon, Craig; Alauddin, Mian M.; Gelovani, Juri G.; Ying, Yunming; Guo, Liwei; Peng, Zhenghong; Yeh, Hsin Hsien
- Abstract
<bold>Introduction: </bold>Previous studies demonstrated that the lactose-binding protein (hepatocellular carcinoma-intestine-pancreas and pancreatitis-associated proteins (HIP/PAP)) is upregulated >130 times in peritumoral pancreatic tissue as compared to normal pancreatic tissue. Therefore, we developed a new radiolabeled ligand of HIP/PAP, the ethyl-β-D-galactopyranosyl-(1,4')-2'-deoxy-2'-[¹⁸F]fluoro-β-D-glucopyranoside (Et-[¹⁸F]FDL) for noninvasive imaging of pancreatic carcinoma using positron emission tomography and computerized tomography (PET/CT).<bold>Methods: </bold>The novel precursor and radiolabeling methods for synthesis of Et-[¹⁸F]FDL produced no isomers; the average decay-corrected radiochemical yield was 68%, radiochemical purity >99%, and specific activity >74 GBq/µmol. The radioligand properties of Et-[¹⁸F]FDL were evaluated using an ex vivo autoradiography and immunohistochemistry in pancreatic tissue sections obtained from mice-bearing orthotopic pancreatic tumor xenografts.<bold>Results and Discussion: </bold>Et-[¹⁸F]FDL binding to peritumoral pancreatic tissue sections strongly correlated with HIP/PAP expression (r = 0.81) and could be completely blocked by treatment with 1 mM lactose.<bold>Conclusion: </bold>These results suggest that Et-[¹⁸F]FDL is a promising agent which should be evaluated for detection of early pancreatic carcinomas by PET/CT imaging.
- Subjects
AUTORADIOGRAPHY; LACTOSE; PANCREATITIS; PANCREATIC cancer; RADIOLIGAND assay; XENOGRAFTS
- Publication
Molecular Imaging & Biology, 2011, Vol 13, Issue 3, p536
- ISSN
1536-1632
- Publication type
journal article
- DOI
10.1007/s11307-010-0334-9